| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
HAEGT targets human dipeptidyl peptidase-IV (DPP-IV), an enzyme that cleaves N-terminal dipeptides from peptides with a proline or alanine at the penultimate position. As a competitive substrate for DPP-IV, HAEGT is used to probe the prime substrate binding sites of the enzyme. The peptide's N-terminal His-Ala is catalytically cleaved by DPP-IV. Through its interaction with DPP-IV, HAEGT is relevant to the study of GLP-1 metabolism, as DPP-IV is the primary enzyme responsible for GLP-1 degradation in vivo. The compound is used in diabetes and obesity research.
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| ln Vitro |
HAEGT (0-500 μM) is a competitive substrate that targets the principal substrate binding site of human dipeptidyl peptidase IV (DPP-IV) [1]. DPP-IV catalyzes the cleavage of HAEGT, with a km value of 38 μM and a Kcat value of 3.1 S-1 [1].
In vitro studies have characterized HAEGT as a competitive substrate for probing prime substrate binding sites of human dipeptidyl peptidase-IV (DPP-IV). The peptide is catalytically cleaved by DPP-IV with a Km value of 38 microM and a Kcat value of 3.1 s-¹. HAEGT (0-500 microM) is used in enzyme kinetic assays to study DPP-IV activity and inhibition. The peptide serves as a quantitative baseline for assay development and inhibitor screening. Its cleavage by DPP-IV provides a model for studying the enzyme's substrate specificity and catalytic mechanism. |
| ln Vivo |
In vivo studies of HAEGT are limited, as the peptide is primarily used as an in vitro research tool. As a fragment of GLP-1, HAEGT is relevant to the study of GLP-1 metabolism and DPP-IV inhibition in the context of diabetes and obesity. The peptide's role as a DPP-IV substrate suggests that in vivo, it would be rapidly cleaved by the enzyme. However, specific in vivo studies using HAEGT have not been extensively reported. The compound is used in research applications to understand DPP-IV biology and to develop DPP-IV inhibitors for therapeutic use.
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| Enzyme Assay |
The in vitro enzyme assay for HAEGT involves incubating the peptide with human dipeptidyl peptidase-IV (DPP-IV) in a suitable buffer system. The reaction is carried out at physiological pH and temperature. Cleavage of the N-terminal His-Ala is monitored using methods such as HPLC, mass spectrometry, or fluorometric detection if a labeled substrate is used. Kinetic parameters including Km (38 microM) and Kcat (3.1 s-¹) are determined from initial velocity measurements at various substrate concentrations. Inhibition studies can be performed by adding DPP-IV inhibitors to the reaction. Data analysis using Michaelis-Menten kinetics yields enzyme kinetic parameters.
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| Cell Assay |
In vitro cellular assays for HAEGT are limited as the peptide is primarily used as a biochemical substrate rather than a cellular probe. For studies involving DPP-IV expressing cells, HAEGT can be added to cell culture media, and its cleavage products can be analyzed to assess cellular DPP-IV activity. Cells expressing DPP-IV, such as intestinal epithelial cells or immune cells, are treated with HAEGT, and the extent of cleavage is measured. The peptide can also be used in cell-based assays to evaluate the efficacy of DPP-IV inhibitors. Cell viability and specificity are confirmed using appropriate controls.
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| Animal Protocol |
In vivo animal studies for HAEGT are not extensively reported, as the peptide is primarily used as an in vitro research tool. As a fragment of GLP-1, HAEGT could potentially be used in animal models of diabetes to study DPP-IV activity. However, the peptide's rapid cleavage by DPP-IV would limit its utility as a stable in vivo probe. For research applications, the compound is typically used in ex vivo assays with tissue samples or in vitro enzyme assays. Standard protocols for DPP-IV activity measurement in plasma or tissue homogenates may employ HAEGT as a substrate.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for HAEGT are not extensively reported. As a 5-amino acid peptide with a molecular weight of 513.5 g/mol, HAEGT is susceptible to rapid degradation by proteases, particularly DPP-IV, which cleaves the N-terminal His-Ala. The peptide is used as a research tool rather than a therapeutic candidate, so comprehensive pharmacokinetic studies have not been conducted. For in vitro assays, the peptide is typically dissolved in aqueous buffers and used immediately. Stability data indicate that the peptide should be stored under appropriate conditions to prevent degradation.
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| Toxicity/Toxicokinetics |
Toxicology data for HAEGT are not extensively reported, as the peptide is a research tool rather than a therapeutic compound. As a 5-amino acid fragment of GLP-1, HAEGT is expected to have low toxicity. Standard safety assessments for research peptides include evaluation of cytotoxicity in cell culture and assessment of potential immunogenicity. However, specific toxicity data, including LD50 values and organ toxicity profiles, are not available. The compound is for research use only and is not intended for human therapeutic applications.
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| References | |
| Additional Infomation |
HAEGT is the first N-terminal 1-5 residues of glucagon-like peptide-1 (GLP-1) with the sequence His-Ala-Glu-Gly-Thr. It has a molecular formula of C20H31N7O9 and a molecular weight of 513.5 g/mol. The peptide is used as a competitive substrate for probing prime substrate binding sites of human dipeptidyl peptidase-IV (DPP-IV), with a Km of 38 microM and a Kcat of 3.1 s-¹. HAEGT is used in the study of diabetes, obesity, and other metabolic diseases. It is designed for biological research and industrial applications.
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| Molecular Formula |
C20H31N7O9
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| Molecular Weight |
513.50164437294
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| Exact Mass |
627.211
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| CAS # |
852155-81-8
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| PubChem CID |
155977576
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
43
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| Complexity |
909
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| Defined Atom Stereocenter Count |
5
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| SMILES |
[C@H](CCC(=O)O)(C(=O)NCC(=O)N[C@H](C(=O)O)[C@H](O)C)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC1NC=NC=1
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| InChi Key |
VBAIGNOKQDKJSE-YPCYXPSQSA-N
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| InChi Code |
InChI=1S/C20H31N7O9.C2HF3O2/c1-9(25-18(33)12(21)5-11-6-22-8-24-11)17(32)26-13(3-4-15(30)31)19(34)23-7-14(29)27-16(10(2)28)20(35)36;3-2(4,5)1(6)7/h6,8-10,12-13,16,28H,3-5,7,21H2,1-2H3,(H,22,24)(H,23,34)(H,25,33)(H,26,32)(H,27,29)(H,30,31)(H,35,36);(H,6,7)/t9-,10+,12-,13-,16-;/m0./s1
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| Chemical Name |
(4S)-4-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-5-[[2-[[(1S,2R)-1-carboxy-2-hydroxypropyl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid;2,2,2-trifluoroacetic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9474 mL | 9.7371 mL | 19.4742 mL | |
| 5 mM | 0.3895 mL | 1.9474 mL | 3.8948 mL | |
| 10 mM | 0.1947 mL | 0.9737 mL | 1.9474 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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